%0 Journal Article
%9 ACL : Articles dans des revues avec comité de lecture répertoriées par l'AERES
%A Marchand, P.
%A Bazin, M. A.
%A Pagniez, F.
%A Riviere, G.
%A Bodero, L.
%A Marhadour, S.
%A Nourrisson, M. R.
%A Picot, C.
%A Ruchaud, S.
%A Bach, S.
%A Baratte, B.
%A Sauvain, Michel
%A Pareja, D. C.
%A Vaisberg, A. J.
%A Le Pape, P.
%T Synthesis, antileishmanial activity and cytotoxicity of 2,3-diaryl- and 2,3,8-trisubstituted imidazo[1,2-a]pyrazines
%D 2015
%L fdi:010065400
%G ENG
%J European Journal of Medicinal Chemistry
%@ 0223-5234
%K Antileishmanial activity ; Imidazo[1,2-a]pyrazines ; Direct arylation ; Casein kinase 1
%M ISI:000363344700032
%P 381-395
%R 10.1016/j.ejmech.2015.09.002
%U https://www.documentation.ird.fr/hor/fdi:010065400
%> https://www.documentation.ird.fr/intranet/publi/2015/11/010065400.pdf
%V 103
%W Horizon (IRD)
%X A series of original 2-phenyl-3-(pyridin-4-yl)imidazo[1,2-a]pyrazines and the 3-iodo precursors, bearing a polar moiety at the C-8 position, was synthesized and evaluated for their antileishmanial activities. Two derivatives exhibited very good activity against the promastigote and the amastigote forms of Leishmania major in the micromolar to submicromolar ranges, coupled with a low cytotoxicity against macrophages and 3T3 mouse fibroblast cells. Through LmCK1 inhibition assay, investigations of the putative molecular target of these promising antileishmanial compounds will be discussed.
%$ 020 ; 052